11777 - Medicinal and Toxicological Chemistry 2

Learning outcomes

At the end of the course the student knows the molecular bases of the drug target interactions; he has knowledge on the therapeutic properties of both natural and synthetic drugs which interact with neurotransmitter receptors of central and peripheral nervous system; he knows the innovative features of drugs recently entered to market or in clinical trials.

Course contents

Drugs Affecting Cholinergic Neurotrasmission.

Acetylcholine neurochemistry. Characterization of acetylcholine receptors.

Nicotinic agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Nicotinic antagonists. Neuromuscolar Blocking Agents. Muscarinic agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Acethylcholinesterase inhibitors. Mechanism of action. Structure-activity Relationships. Muscarinic antagonists. Mechanism of action. Structure-activity Relationships.

Drugs Affecting Adrenergic Neurotrasmission.

Biosynthesis, metabolism and function of norepinephrine and epinephrine. Characterization of adrenergic receptor subtypes. Therapeutic relevance of adrenergic receptor subtypes.

a1 and a2-adrenergic Agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. a-adrenergic Antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Drugs affecting catecholamine biosynthesis, storage, reuptake and metabolism. Therapeutic application. Mechanism of action. Structure-activity Relationships. b-adrenergic Agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. b-adrenergic Antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships.

Drugs Affecting Dopaminergic Neurotrasmission.

Biosynthesis, metabolism and function of dopamine. Characterization of dopaminergic receptors. Therapeutic relevance of dopaminergic receptors.

Dopaminergic receptor Antagonists. Phenothiazine and thioxantene neuroleptics. Mechanism of action. Structure-activity Relationships. Butyrophenone neuroleptics. Mechanism of action. Structure-activity Relationships. Benzamide neuroleptics. Mechanism of action. Structure-activity Relationships. Benzisoxazoles neuroleptics. Mechanism of action. Structure-activity Relationships.

Drugs Affecting Serotoninergic Neurotrasmission.

Biosynthesis, metabolism and function of serotonin. Characterization of serotonin receptor subtypes.

5HT1A agonists. Therapeutic application. Mechanism of action. 5HT1D agonists. Therapeutic application. Mechanism of action. 5HT2A agonists. Therapeutic application. Mechanism of action. 5HT2A antagonists. Therapeutic application (Antipsychotic agents and antidepressants). Mechanism of action. 5HT2A antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Serotonin re-uptake inhibitors (SSRIs). Therapeutic application (antidepressants). Mechanism of action.

Drugs Acting on GABAA receptor complex.

Biosynthesis, metabolism and function of gamma-aminobutiric acid. Benzodiazepines (Anxiolytics). Therapeutic application. Mechanism of action. Structure-activity Relationships. Metabolism.

Drugs Affecting Histamine Neurotrasmission. Histamine biosynthesis, catabolism and function. Characterization of histamine receptors. H1 receptor antagonists (first and second generation). Therapeutic application. Mechanism of action. Structure-activity Relationships. H2 receptor antagonists (antiulcer agents). Therapeutic application. Mechanism of action. Structure-activity Relationships.

Drugs Acting on Opioid Receptors.

Endogenous opioid peptides. Fisiological functions. Characterization of opioid receptors.

Opioid receptor agonists (analgesics). Therapeutic application. Mechanism of action. Mixed agonist-antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships.

Readings/Bibliography

David A. William, Thomas L. Lemke, Foye's Priciples of Medicinal Chemistry, Lippincott Williams & Wilkins Publishers, Fifth Edition.

Slides and note from lessons.

Teaching methods

Assessment methods

The final examination is an oral discussion comprising a  series of questions that aim to ascertain students' understanding of the subject presented during lectures.

Teaching tools

Videoprojector, PC.

Office hours

See the website of Marinella Roberti